Diarrhea antidiarrheals

The dangers of dependency and addiction clearly preclude the use of such compounds as morphine, meperidine, and methadone as treatment for diarrhea. Antidiarrheal specificity therefore is of paramount importance in choosing among the synthetic opioids and their analogues (e.g., diphenoxylate and loperamide). 

Increased motility of the gastrointestinal tract and decreased absorption of fluid are major factors in diarrhea. Antidiarrheal drugs include antimotility agents, adsorbents, and drugs that modify fluid and electrolyte transport (Figure 24.8). 

Diagnosis and alleviation of the cause, if possible, is of primary importance. Often, however, this is not possible and therapy is used to alleviate the inconvenience and pain of diarrhea. These compounds usually only mask the underlying factors producing the problem. Diarrhea may cause significant dehydration and loss of electrolytes and is a particularly serious problem in infants. Antidiarrheals do not usually prevent the loss of fluids and electrolytes into the large bowel and, although these may prevent frequent defecation, often the serious imbalance of body electrolytes and fluids is not significantly affected. 

When an opiate is used as an antidiarrheal drug, the nurse records each bowel movement, as well as its appearance, color, and consistency. The nurse should notify the primary health care provider immediately if diarrhea is not relieved or becomes worse if die patient has severe abdominal pain or if blood in die stool is noted. 

Antidiarrheals decrease intestinal peristalsis, which is usually increased when the patient has diarrhea. Examples of these drug s include difenoxin with atropine (Motofen), diphenoxylate witii atropine (Lomotil), and loperamide (Imodium). 

These drugs are contraindicated in patients whose diarrhea is associated witii organisms that can harm the intestinal mucosa (Escherichia coli, Salmonella, Shigella) and in patients with pseudomembranous colitis, abdominal pain of unknown origin, and obstructive jaundice The antidiarrheal drugs are contraindicated in children younger than 2 years. 

ANTIDIARRHEALS. The nurse notifies the primary health care provider if an elevation in temperature occurs or if severe abdominal pain or abdominal rigidity or distention occurs because this may indicate a complication of the disorder, such as infection or intestinal perforation. If diarrhea is severe, additional treatment measures, such as IV fluids and electrolyte replacement, may be necessary. 

Educate the patient about (1) the causes of acute and chronic diarrhea (2) the possible complications of diarrhea (3) the goals of treatment for diarrhea (4) the antidiarrheal medication used to manage acute or chronic diarrhea and (5) if appropriate, the circumstances when antibiotics are used to treat diarrhea. 

R. C., et al., Quantitative, non-invasive assessment of antidiarrheal actions of codeine using an experi-mental model of diarrhea in man, Dig. Dis. Sci. 1993, 38, 996-1003. 

The most frequently observed symptoms include vomiting (82%), nausea (74%), abdominal cramps (64%), diarrhea (64%), and also headaches and muscular cramping. The onset of symptoms usually starts after 6 to 10 hours after food ingestion, however they may be reported earlier. The lethal cases are rare and occur among infants and elderly people. Only 10% of affected people need medical treatment - treatments include analgesics, antidiarrheic drugs, and administration of fluids. 

A not uncommon side effect observed with morphine and some of the other narcotic analgesics is constipation due to decreased motility of the gastrointestinal tract. It proved possible to so modify pethidine as to retain the side effect at the expense of analgesic activity. Relief of diarrhea, it will be realized, is a far from trivial indication. Alkylation of the anion from diphenylacetonitrile (95) with ethylene dibromide gives the intermediate, 96. Alkylation of normeperidine (81) with that halide affords diphenoxylate (97), an antidiarrheal agent. 

Loperamide is presently used more often as an antidiarrheal drug than as an analgesic, and it is also included in the list of over-the-counter drugs because of its insignificant action on the CNS. It reduces intestinal smooth muscle tone and motility as a result of binding to intestinal opiate receptors. It is used for symptomatic treatment of severe and chronic diarrhea of various origins. The most popular synonym for loperamide is imodium. 

Nonspecific antidiarrheal agents may be useful in treating self-limiting diarrhea. Kaolin and pectin or chalk may adsorb noxious compounds but evidence that such adsorbents are effective is unconvincing. Disadvantages can be prolongation of the course of infection and interference with absorption of desired drugs. 

Colestyramine bind bile acids in the large bowel and is an effective antidiarrheal agent when high concentrations of bile acids are the cause of the diarrhea. 

Antidiarrheal activity. Decoction of the dried rhizome, taken orally hy children, was active. Infantile diarrhea was treated with kexieding capsule composed of 5 plant materials, including roasted ginger, clove, and fruit peel of Punica granatum. Of the 234 infants and 71 children treated, 281 (92%) were cured in 1-3 days and 9 (3%) were significantly improved. The total effective rate was 95% . Water extract of the dried rhizome, administered hy gastric intubation to mice at a dose of 0.5 mg/g, was active vs castor oil-induced diarrhea . 

Consume small, frequent meals to help offset nausea and vomiting consider taking OTC antidiarrheals if diarrhea occurs... 

Notify fhe physician if severe diarrhea occurs and avoid taking antidiarrheals until directed to do so... 

For the treatment of diarrhea, 15 to 30 mg of codeine is typically given two to three times per day until bowel movements return to normal. Because of the risk of addiction, however, codeine as an antidiarrheal drug is dispensed sparingly. Constipation (the opposite of diarrhea—there is no movement) is considered an unwanted side effect of codeine when it is used for its analgesic effect. (This is discussed in Chapter 4.)... 

The most common adverse effects associated with nelfinavir are diarrhea and flatulence. Diarrhea often responds to antidiarrheal medications but can be dose-limiting. Nelfinavir is an inhibitor of the CYP3A system, and multiple drug interactions may occur (Tables 49-3 and 49-4). An increased dosage of nelfinavir is recommended when co-administered with rifabutin (with a decreased dose of rifabutin), whereas a decrease in saquinavir dose is suggested with concurrent nelfinavir. Co-administration with efavirenz should be avoided due to decreased indinavir levels. Nelfinavir has a favorable safety and pharmacokinetic profile for pregnant women compared with that of other Pis (Table 49-5) there is no evidence of human teratogenicity. 

Antidiarrheal agents may be used safely in patients with mild to moderate acute diarrhea. However, these agents should not be used in patients with bloody diarrhea, high fever, or systemic toxicity because of the risk of worsening the underlying condition. They should be discontinued in patients whose diarrhea is worsening despite therapy. Antidiarrheals are also used to control chronic diarrhea caused by such conditions as irritable bowel syndrome (IBS) or inflammatory bowel disease (IBD). 

Antidiarrheal agents Bismuth subsalicylate, 524 mg every 30-60 minutes as needed up to 8 doses daily Kaopectate, Pepto- Bismol, various generics Antidiarrheals should not be used if diarrhea is accompanied by fever > 101°F or if blood or mucus is present in stool. Bismuth salts can cause dark discoloration of the tongue and stools. Salicylates are absorbed and can cause tinnitus if coadministered with aspirin. 

Shook, J.E., Lemcke, P.K., Gehrig, C.A., Hruby, V.J., Burks, T.F. Antidiarrheal properties of supraspinal mu and delta and peripheral mu, delta and kappa opioid receptors inhibition of diarrhea without constipation, J. Pharmacol. Exp. Ther. 1989, 249, 83-90. 

Despite the lack of studies correlating the antidiarrheic activity of crude drugs with the presence of flavonoids, these have been also studied as pure compounds in this regard. The most used assay of antidiarrhoeic activity is the castor oil test, in which diarrhea is induced by the oral administration of castor oil to mice. Different flavonoids have been shown to possess antidiarrheal activity in this test quercetin, kaempferol, morin, myricetin, rutin (i.p.) [117,118], quercitrin (p.o.) [114,119], and tematin (i.p.) [44], all showing a dose-dependent activity in the range between 25 and 100 mg/kg. However, flavonoids are not only able to exert a preventive antidiarrheal effect in this acute model of experimentally-induced diarrhea, but also in chronic models. Thus quercitrin showed beneficial effects in a model of lactose-induced chronic diarrhea in rats, since it reduced the diarrheal output and facilitated colonic mucosal repair in lactose fed [120]. 

Ippoliti C. Antidiarrheal agents for the management of treatment-related diarrhea in cancer patients. Am J Health SystPharm. 1998 55 1573-1580. 

Avens is stated to possess antidiarrheal, antihemorrhagic, and febrifugal properties. It is used for diarrhea, catarrhal colitis, passive uterine hemorrhage, intermittent fevers, and particularly for ulcerative colitis. 

Cassia is stated to possess carminative, antispasmodic, antiemetic, antidiarrheal, and antimicrobial properties. It has been used to treat flatulent dyspepsia, flatulent colic, diarrhea, the common cold, and especially colic or dyspepsia with flatulent distension and nausea. Cassia bark is also documented to possess astringent properties, and the oil has carminative and antiseptic characteristics. 

Cinnamon is believed to have antispasmodic, carminative, orexigenic, antidiarrheal, antimicrobial, refrigerant, and anthelmintic properties. It is used for anorexia, intestinal colic, infantile diarrhea, common cold, influenza, and specifically for flatulent colic and dyspepsia with nausea. Cinnamon bark is also an astringent, and cinnamon oil is reported to possess carminative and antiseptic properties. 

Cola is believed to have central nervous system (CNS)-stimulant, thymoleptic, antidepressant, diuretic, cardioactive, and antidiarrheal properties. It is used to treat depressive states, melancholy, atony, exhaustion, dysentery, atonic diarrhea, anorexia, migraine, and particularly depressive states associated with general muscular weakness. 

Diphenoxylate and its metabolite, difenoxin, are not used for analgesia but for the treatment of diarrhea. They are scheduled for minimal control (difenoxin is schedule IV, diphenoxylate schedule V see inside front cover) because the likelihood of their abuse is remote. The poor solubility of the compounds limits their use for parenteral injection. As anti diarrheal drugs, they are used in combination with atropine. The atropine is added in a concentration too low to have a significant antidiarrheal effect but is presumed to further reduce the likelihood of abuse. 

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